CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt.
CHMFL-KIT-031 also displays 15-400-fold selectivity over other primary mutants such as L576P and secondary mutants including T670I, V654A as well as N822K and D816V.
CHMFL-KIT-031 exhibits a selectivity S score (1) of 0.01 among 468 kinases/mutants in the KINOMEScan™ assay.
CHMFL-KIT-031 inhibits the proliferation of BaF3-TEL-KIT-V559D cells with IC50 of 25 nM, shows potent inhibitory efficacy for KIT V559D mediated signaling pathways in cell and anti-tumor activity in vivo.
